AS703026
1236699-92-5
99%
2026-07-19
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName AS703026 Cat No CEI-0153 Description As a novel, selective, orally bioavailable inhibitor, AS703026 can inhibit MEK1/2 with IC50 of with IC50 of 5-11 nM. Alias MSC1936369B CAS No 1236699-92-5 Molecular Weight 431.2 Purity >99% Storage 2 years at -20 centigrade Synonyms MSC1936369B Targets MEK1/2 Molecular Formula C15H15FIN3O3 Chemical Name (S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylamino)isonicotinamide Solubility DSMO 86 mg/mL Water In vitro As a novel, selective, orally bioavailable inhibitor, AS703026 can inhibit MEK1/2 with IC50 of with IC50 of 5-11 nM. For cell lines, (1)AS703026 effectively inhibited the growth of D-MUT cells in vitro and in vivo by specific inhibition of the key MEK downstream target kinase ERK. Inhibition of MEK by AS703026 suppressed cetuximab-resistant colorectal cancer cells attributed to K-ras mutation both in vitro and in vivo. (2)AS703026 also inhibit growth and survival of MM (human multiple myeloma) cells and cytokine-induced osteoclast differentiation more potently (9- to 10-fold) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression. AS703026 further induced apoptosis via caspase 3 and Poly ADP ribose polymerase (PARP) cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs). In vivo AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. Significant tumour growth reduction in AS703026- vs. vehicle-treated mice bearing H929 MM xenograft tumours correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels in vivo. AS703026, at the concentration less than 200 nM, was cytotoxic against the majority of tumour cells tested from patients with relapsed and refractory MM, regardless of mutational status of RAS and BRAF genes. category Heterocyclic Compound(c1111) cas_num 1236699-92-5 Basic Info-
Product Name:
AS703026
Other Name:AS703026;N-[(2S)-2,3-Dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]-4-pyridinecarboxamide;(S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylaMino)isonicotinaMide;4-PyridinecarboxaMide, N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)aMino]-;MSC1936369B;PiMasertib (AS-703026);AS703026/MSC1936369B;PiMasertib
CAS No.:1236699-92-5
Molecular Formula:C15H15FIN3O3
InChIKeys:VIUAUNHCRHHYNE-JTQLQIEISA-N
Molecular Weight:431.2007732
Exact Mass:431.014191
Categories:
Characteristics-
PSA:
94.5
XLogP3:1.7
Density:1.769
Flash Point:330.7±31.5 °C
Refractive Index:1.684
Hazard IdentificationClassification of the substance or mixture
no data available
GHS label elements, including precautionary statements
Pictogram(s) no data available Signal word no data available
Hazard statement(s) no data available
Precautionary statement(s) Prevention no data available
Response no data available
Storage no data available
Disposal no data available
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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